公开(公告)号：US20080119548A1

公开(公告)日：2008-05-22

申请号：US10593090

申请日：2005-03-18

申请人： Gabrielle V. Ronnett ,  Frankcis P. Kuhajda ,  Jagan N. Thupari ,  Leslie E. Landree ,  Timothy H. Moran ,  Eun-Kyoung Kim

发明人： Gabrielle V. Ronnett ,  Frankcis P. Kuhajda ,  Jagan N. Thupari ,  Leslie E. Landree ,  Timothy H. Moran ,  Eun-Kyoung Kim

IPC分类号： A61K31/341 ,  A61P3/04

CPC分类号： A61K31/34 ,  A61K31/70

摘要： Obesity is a worldwide health issue, affecting children and adults in developed and developing countries. Obesity is a disorder of both energy metabolism and appetite regulation, and may be understood as a dysfunction of energy balance. Applicants have found a means for regulating food intake by a subject by administering a compound to the subject which affects neuronal energy balance. Applicants have found a means for regulating food intake by a subject administering a compound to the subject which targets the activity of AMPK, in particular inhibiting activation, in particular hypothalamic. Applicants have also found a method of inducing weight loss in a subject by decreasing the subjects appetite by administering a compound to the subject which increases the subject's neuronal energy balance.

摘要翻译： 肥胖是世界卫生问题，影响发达国家和发展中国家的儿童和成人。 肥胖是能量代谢和食欲调节的障碍，可以理解为能量平衡的功能障碍。 申请人已经发现通过向受试者施用影响神经元能量平衡的化合物来调节受试者的食物摄取的方法。 申请人已经找到一种方法来调节受试者施用靶向AMPK活性的化合物，特别是抑制活化，特别是下丘脑的化合物的摄食。 申请人还发现通过向受试者施用增加受试者的神经元能量平衡的化合物，通过降低受试者的食欲来诱导受试者体重减轻的方法。

公开(公告)号：US20090124684A1

公开(公告)日：2009-05-14

申请号：US12266425

申请日：2008-11-06

申请人： Jagan N. Thupari ,  Leslie E. Landree ,  Gabrielle Ronnett ,  Francis P. Kuhajda

发明人： Jagan N. Thupari ,  Leslie E. Landree ,  Gabrielle Ronnett ,  Francis P. Kuhajda

IPC分类号： A61K31/381 ,  A61K31/365 ,  C12Q1/48

CPC分类号： A61K31/00 ,  A23L33/10 ,  A23L33/175 ,  A23L33/40 ,  A61K31/195 ,  A61K31/198 ,  A61K31/205 ,  A61K31/34 ,  A61K31/365 ,  A61K31/381 ,  C12Q1/48 ,  G01N2500/04

摘要： This invention provides methods and compositions for inducing weight loss and maintaining optimum weight comprising administering an agent that stimulates carnitine palmitoyl transferase-1 (CPT-1) activity to the patient in need, including human patients. These methods do not require inhibition of fatty acid synthesis. In particular, this invention provides methods for development of therapeutics that selectively enhance fatty acid oxidation, increase energy production, and reduce adiposity while preserving lean mass, through the pharmacological stimulation of CPT-1 activity. In a preferred mode, the agent is administered in an amount sufficient to increase fatty acid oxidation. In another preferred mode, the agent is administered in an amount sufficient to antagonize malonyl CoA inhibition of CPT-1. In yet another preferred mode, the agent is administered in an amount sufficient to increase malonyl CoA level.

摘要翻译： 本发明提供用于诱导体重减轻和保持最佳重量的方法和组合物，包括向需要的患者（包括人类患者）施用刺激肉碱棕榈酰转移酶-1（CPT-1）活性的药剂。 这些方法不需要抑制脂肪酸合成。 特别地，本发明提供了通过CPT-1活性的药理学刺激来开发选择性增强脂肪酸氧化，增加能量产生和减少肥胖同时保持瘦体重的治疗剂的方法。 在优选的方式中，给药剂量足以增加脂肪酸氧化。 在另一种优选方式中，给药剂量足以拮抗CPT-1的丙二酰辅酶A抑制。 在又一优选方式中，给药剂量足以增加丙二酰辅酶A水平。